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BG99593A - Application of dtmethylbenzofurans as 5-ht3 antagonists - Google Patents

Application of dtmethylbenzofurans as 5-ht3 antagonists

Info

Publication number
BG99593A
BG99593A BG99593A BG9959395A BG99593A BG 99593 A BG99593 A BG 99593A BG 99593 A BG99593 A BG 99593A BG 9959395 A BG9959395 A BG 9959395A BG 99593 A BG99593 A BG 99593A
Authority
BG
Bulgaria
Prior art keywords
pct
date jun
represents hydrogen
sec
formula
Prior art date
Application number
BG99593A
Other languages
Bulgarian (bg)
Other versions
BG62489B1 (en
Inventor
Daele Georges Van
Jean-Paul Bosmans
Laerhoven Willy Van
Original Assignee
Janssen Pharmaceutica N.V.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Janssen Pharmaceutica N.V. filed Critical Janssen Pharmaceutica N.V.
Publication of BG99593A publication Critical patent/BG99593A/en
Publication of BG62489B1 publication Critical patent/BG62489B1/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/26Psychostimulants, e.g. nicotine, cocaine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/56Nitrogen atoms
    • C07D211/58Nitrogen atoms attached in position 4
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Addiction (AREA)
  • Otolaryngology (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Furan Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Steroid Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyrane Compounds (AREA)
  • Dental Preparations (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

PCT No. PCT/EP93/03206 Sec. 371 Date Jun. 16, 1995 Sec. 102(e) Date Jun. 16, 1995 PCT Filed Nov. 15, 1993 PCT Pub. No. WO94/12494 PCT Pub. Date Jun. 9, 1994Method of treating 5-HT3-mediated disorders, which comprises systemic administration of an effective amount of a compound of formula (I) <IMAGE> (I) the pharmaceutically acceptable acid addition salt forms and the stereochemically isomeric forms thereof, wherein R1 and R2 represent hydrogen, or R1 and R2 taken together form a bivalent radical of formula -CH=CH-CH=CH- (a), -CH=C(Cl)-CH=CH- (b) or -CH=CH-C(Cl)=CH- (c); n represents 2, 3 or 4; R3 represents hydrogen or methoxy; m represents 1 or 2; R4 represents hydrogen, amino or C1-3-alkylcarbonylamino; and R5 represents hydrogen or halo; novel compounds; compositions; processes for preparing novel compounds and intermediates.
BG99593A 1992-11-20 1995-04-20 Application of dimethylbenzofurans as 5-ht3 antagonists BG62489B1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US97901392A 1992-11-20 1992-11-20
PCT/EP1993/003206 WO1994012494A1 (en) 1992-11-20 1993-11-15 Use of dimethylbenzofurans and dimethylbenzopyrans as 5-ht3 antagonists

Publications (2)

Publication Number Publication Date
BG99593A true BG99593A (en) 1995-12-29
BG62489B1 BG62489B1 (en) 1999-12-30

Family

ID=25526607

Family Applications (1)

Application Number Title Priority Date Filing Date
BG99593A BG62489B1 (en) 1992-11-20 1995-04-20 Application of dimethylbenzofurans as 5-ht3 antagonists

Country Status (31)

Country Link
US (2) US5674868A (en)
EP (1) EP0669919B1 (en)
JP (1) JP2830952B2 (en)
KR (1) KR0166661B1 (en)
AT (1) ATE176232T1 (en)
AU (1) AU680640B2 (en)
BG (1) BG62489B1 (en)
BR (1) BR9307477A (en)
CA (1) CA2149044C (en)
CZ (1) CZ287262B6 (en)
DE (1) DE69323322T2 (en)
DK (1) DK0669919T3 (en)
ES (1) ES2129615T3 (en)
FI (1) FI952458A (en)
GR (1) GR3029831T3 (en)
HU (2) HUT72740A (en)
IL (3) IL107654A (en)
LV (1) LV10956B (en)
MX (1) MX9307257A (en)
NO (2) NO307690B1 (en)
NZ (1) NZ257854A (en)
OA (1) OA10158A (en)
PL (1) PL176051B1 (en)
RO (1) RO115160B1 (en)
RU (1) RU2116072C1 (en)
SG (1) SG47488A1 (en)
SK (1) SK282378B6 (en)
TW (1) TW294595B (en)
UA (1) UA49792C2 (en)
WO (1) WO1994012494A1 (en)
ZA (1) ZA938676B (en)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5374637A (en) * 1989-03-22 1994-12-20 Janssen Pharmaceutica N.V. N-(3-hydroxy-4-piperidinyl)(dihydrobenzofuran, dihydro-2H-benzopyran or dihydrobenzodioxin)carboxamide derivatives
DE69816060T2 (en) 1997-04-18 2004-04-22 Janssen Pharmaceutica N.V. USE OF 5HT3 ANTAGONISTS TO PROMOTE THE COLON
EP1000029B1 (en) * 1997-07-11 2003-10-01 Janssen Pharmaceutica N.V. (+)-norcisapride useful for 5-ht3 and 5-ht4 mediated disorders
US6239122B1 (en) * 2000-01-05 2001-05-29 Joy Ann Steele Method of treatment of nausea, vomiting, and other disorders using estrogens
WO2004111014A1 (en) * 2003-06-06 2004-12-23 Vertex Pharmaceuticals Incorporated Pyrimidine derivatives as modulators of atp-binding cassette transporters
CA2546002C (en) 2003-11-20 2012-09-18 Janssen Pharmaceutica N.V. 7-phenylalkyl substituted 2-quinolinones and 2-quinoxalinones as poly(adp-ribose) polymerase inhibitors
US7855207B2 (en) 2003-11-20 2010-12-21 Janssen Pharmaceutica, Nv 6-alkenyl and 6-phenylalkyl substituted 2-quinolinones and 2-quinoxalinones as poly(adpribose) polymerase inhibitors
CA2569824C (en) 2004-06-30 2013-03-19 Janssen Pharmaceutica N.V. Phthalazine derivatives as parp inhibitors
EA012416B1 (en) 2004-06-30 2009-10-30 Янссен Фармацевтика Н.В. Substituted 2-alkyl quinazolinone derivatives as parp inhibitors
CA2569827C (en) 2004-06-30 2013-04-09 Janssen Pharmaceutica N.V. Quinazolinedione derivatives as parp inhibitors
EP2134691B1 (en) 2007-03-08 2012-01-25 Janssen Pharmaceutica, N.V. Quinolinone derivatives as parp and tank inhibitors
US8404713B2 (en) 2007-10-26 2013-03-26 Janssen Pharmaceutica Nv Quinolinone derivatives as PARP inhibitors
CA2716088C (en) 2008-03-27 2017-03-07 Eddy Jean Edgard Freyne Quinazolinone derivatives as tubulin polymerization inhibitors
EP2271626B1 (en) 2008-03-27 2014-11-26 Janssen Pharmaceutica, N.V. Tetrahydrophenanthridinones and tetrahydrocyclopentaquinolinones as parp and tubulin polymerization inhibitors

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA1183847A (en) * 1981-10-01 1985-03-12 Georges Van Daele N-(3-hydroxy-4-piperidinyl)benzamide derivatives
ZW12187A1 (en) * 1986-07-03 1989-02-01 Janssen Pharmaceutica Nv 4-(aroylamino)piperidinebutanamide derivatives
CA1317940C (en) * 1987-09-25 1993-05-18 Georges H. P. Van Daele Substituted n-(1-alkyl-3-hydroxy-4-piperidinyl)benzamides
US5374637A (en) * 1989-03-22 1994-12-20 Janssen Pharmaceutica N.V. N-(3-hydroxy-4-piperidinyl)(dihydrobenzofuran, dihydro-2H-benzopyran or dihydrobenzodioxin)carboxamide derivatives
GB9005014D0 (en) * 1990-03-06 1990-05-02 Janssen Pharmaceutica Nv N.(4.piperidinyl)(dihydrobenzofuran or dihydro.2h.benzopyran)carboxamide derivatives

Also Published As

Publication number Publication date
MX9307257A (en) 1994-05-31
HU9501476D0 (en) 1995-07-28
NZ257854A (en) 1997-04-24
US5863923A (en) 1999-01-26
IL107654A (en) 1998-01-04
IL119273A (en) 2000-07-16
NO995762D0 (en) 1999-11-24
DE69323322D1 (en) 1999-03-11
JPH08505840A (en) 1996-06-25
ATE176232T1 (en) 1999-02-15
RU2116072C1 (en) 1998-07-27
IL119273A0 (en) 1996-12-05
FI952458A0 (en) 1995-05-19
NO307690B1 (en) 2000-05-15
RO115160B1 (en) 1999-11-30
KR0166661B1 (en) 1999-01-15
HU211546A9 (en) 1995-12-28
NO951980L (en) 1995-05-19
PL176051B1 (en) 1999-03-31
UA49792C2 (en) 2002-10-15
SK67595A3 (en) 1995-11-08
EP0669919A1 (en) 1995-09-06
WO1994012494A1 (en) 1994-06-09
BR9307477A (en) 1999-06-29
NO995762L (en) 1995-05-19
IL107654A0 (en) 1994-02-27
OA10158A (en) 1996-12-18
LV10956B (en) 1996-10-20
JP2830952B2 (en) 1998-12-02
HUT72740A (en) 1996-05-28
SG47488A1 (en) 1998-04-17
FI952458A (en) 1995-05-19
BG62489B1 (en) 1999-12-30
DE69323322T2 (en) 1999-09-09
TW294595B (en) 1997-01-01
EP0669919B1 (en) 1999-01-27
SK282378B6 (en) 2002-01-07
LV10956A (en) 1995-12-20
RU95113434A (en) 1997-03-10
CA2149044C (en) 2007-04-03
CZ287262B6 (en) 2000-10-11
CZ125895A3 (en) 1995-10-18
NO951980D0 (en) 1995-05-19
AU680640B2 (en) 1997-08-07
GR3029831T3 (en) 1999-06-30
ES2129615T3 (en) 1999-06-16
DK0669919T3 (en) 1999-09-13
CA2149044A1 (en) 1994-06-09
PL309045A1 (en) 1995-09-18
ZA938676B (en) 1995-05-19
AU5465994A (en) 1994-06-22
US5674868A (en) 1997-10-07
NO308530B1 (en) 2000-09-25

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